Synthesis and Properties of Methyl-, Formyl- and Amino-Diazaphenanthrene

1994 ◽  
Vol 47 (11) ◽  
pp. 2129 ◽  
Author(s):  
L Chrzastek ◽  
B Mianowska ◽  
W Sliwa

Methyl, formyl and amino derivatives of the isomeric benzo [c][1,5] naphthyridine and benzo [f][1,7] naphthyridine have been obtained, and their structures confirmed by 1H n.m.r. spectroscopy. Biological activity data (MIC) for some methyl and formyl derivatives are presented.

2006 ◽  
Vol 42 (3) ◽  
pp. 322-324 ◽  
Author(s):  
M. I. Merlani ◽  
L. Sh. Amiranashvili ◽  
K. G. Mulkidzhanyan ◽  
E. P. Kemertelidze

2018 ◽  
pp. 215-222
Author(s):  
Габиден (Gabiden) Маратович (Maratovich) Байсаров (Baysarov) ◽  
Айдана (Аjdana) Рахманиякызы (Rakhmaniyakyzy) Жуматаева (Zhumatayeva) ◽  
Гулим (Gulim) Кенесбековна (Kenesbekovna) Мукушева (Mukusheva) ◽  
Эльвира (El'vira) Эдуардовна (Eduardovna) Шульц (Shul'ts) ◽  
Роза (Roza) Батталовна (Battalovna) Сейдахметова (Seydakhmetova) ◽  
...  

As a result of complex chemical processing of medicinal raw materials of Artemisia glabella Kar. et Kir., including CO2 extraction and lactones isolation, we have investigated the chemical composition of flavonoids to select the biologically active ones and carry out modifications on their basis. Two flavonoids pectolinaringenin and cirsilineol have been isolated by partition chromatography from the secondary raw materials of Artemisia glabella Kar. et. Kir. and identified. To obtain new biologically active compounds, we have synthesized new amino derivatives of cirsilineol by the Mannich reaction with secondary amines (piperidine and N-methylpiperazine) in isopropanol with the presence of dimethylaminopyridine. In proton NMR spectrum of the synthesized compounds there are proton signals of the initial cirsilineol fragment; however, there is no N-8 proton signal, besides other signals typical for amines’ benzene ring have been observed at 1.53–3.90 ppm. It means that reaction occurred at the C-8 position of carbon in ring A. The synthesized compounds have been studied for various types of biological activity typical for this class, including hepatoprotective and anti-inflammatory activities. Amino derivatives of cirsilineol exhibit a moderate activity against HepG2 cell line, while cirsilineol at a dose of 5 mg/ml expresses a pronounced hepatoprotective activity. Moreover, all samples at a dose of 25 mg/kg show poor anti-inflammatory effects on the model of acute exudative reaction in vivo.


2021 ◽  
Vol 17 ◽  
pp. 558-568
Author(s):  
Zbigniew Malinowski ◽  
Emilia Fornal ◽  
Agata Sumara ◽  
Renata Kontek ◽  
Karol Bukowski ◽  
...  

Amino- and polyaminophthalazinones were synthesized by the palladium‐catalyzed amination (alkyl- and arylamines, polyamines) of 4-bromophthalazinones in good yields. The coordinating properties of selected aminophthalazinones towards Cu(II) ions were investigated and the participation of the nitrogen atoms in the complexation of the metal ion was shown. A biological screening of the potential cytotoxicity of selected synthesized compounds on HT-29 and PC-3 cell lines, as well as on the L-929 cell line, proved that some amino derivatives of phthalazinone show interesting anticancer activities. The detailed synthesis, spectroscopic data, and biological assays are reported.


1996 ◽  
Vol 39 (13) ◽  
pp. 2586-2593 ◽  
Author(s):  
Mao-Chin Liu ◽  
Tai-Shun Lin ◽  
Joseph G. Cory ◽  
Ann H. Cory ◽  
Alan C. Sartorelli

1973 ◽  
Vol 21 (3) ◽  
pp. 609-615 ◽  
Author(s):  
HYOZO TANIYAMA ◽  
YOSUKE SAWADA ◽  
SHIGEO TANAKA

2015 ◽  
Vol 21 (1) ◽  
Author(s):  
Mariola Napiórkowska ◽  
Marcin Cieślak ◽  
Julia Kaźmierczak-Barańska ◽  
Karolina Królewska ◽  
Aleksandra Czapla ◽  
...  

AbstractA series of 38 new derivatives of cyclic imides containing silicon in the structure was synthesized and characterized by


2019 ◽  
Vol 8 (2) ◽  
pp. 11-15
Author(s):  
L. V. Spatlova

Introduction. In recent years, interest in the compounds of the benzofuroxane series has increased, because they have a wide range of biological activity, and in addition are donors of nitric oxide. In the scientific literature, many works are related to the synthesis and study of the biological activity of 5-nitro-4,6-dichlorobenzofuroxane amino derivatives, whereas amino derivatives of the 5,7-dichlor-4,6-dinitrobenzofuroxane substrate have been poorly studied.Aim. Is the synthesis of new amino derivatives of 5,7-dichloro-4,6-dinitrobenzofuroxane and the study of their biological activity.Materials and methods. Investigated the reaction of condensation of 5,7-dichloro-4,6-dinitrobenzofuroxane with different aromatic amines, containing functional groups of acceptor character in their structure were selected. In order to increase the yield for each specific reaction, the reaction conditions were selected (the reaction temperature, medium, and the amount of amine). The structure of the compounds confirmed IR, NMR spectra and elemental analysis.Results and discussion. New compounds in the 5,7-diamino-4,6-dinitrobenzofuroxane series were obtained. Acute toxicity, acaricidal and bacteriostatic activity against Escherichia coli and Staphylococcus aureus were studied. The obtained compounds were found to have high pharmacological activity, superior to the comparison drug (Chlorophos and Creolin).Conclusion. Most of the amino derivative synthesized 5,7-dichloro-4,6-dinitrobenzofuroxane have a high activity against mites and bacteria. Compounds containing in their structure chlorine and methyl radicals, have biological activity at low concentrations, are low-toxic and belong to the 4th hazard class.


ChemInform ◽  
2010 ◽  
Vol 27 (39) ◽  
pp. no-no
Author(s):  
M.-C. LIU ◽  
T.-S. LIN ◽  
J. G. CORY ◽  
A. H. CORY ◽  
A. C. SARTORELLI

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 368
Author(s):  
Ola A. Abu Ali ◽  
Hosam A. Saad ◽  
Bodor M. A. Al Malki

To date, no fused heterocycles have been formed on folic acid molecules; for this reason, and others, our target is to synthesize new derivatives of folic acid as isolated or fused systems. Folic acid 1 reacted with ethyl pyruvate, triethyl orthoformate, ethyl chloroformate, thioformic acid hydrazide, and aldehydes to give new derivatives of folic acid 2–6a,b. Moreover, It reacted with benzylidene malononitrile, acetylacetone, ninhydrin, ethyl acetoacetate, ethyl cyanoacetate, and ethyl chloroacetate to give the pteridine fused systems 10–15, respectively. Ethoxycarbonylamino derivate 5 reacted with some nucleophiles containing the NH2 group, such as aminoguanidinium hydrocarbonate, hydrazine hydrate, glycine, thioformic acid hydrazide, and sulfa drugs in different conditions to give the urea derivatives 16–20a,b. Compound 4 reacted with the same nucleophiles to give the methylidene amino derivatives 21–24a,b. The fused compound 10 reacted with thioglycolic acid carbon disulfide, malononitrile, and formamide to give the four cyclic fused systems 25–30, respectively. The biological activity of some synthesized showed moderate effect against bacteria, but no effect shown towards fungi.


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